- Synthesis and pharmacological evaluation of benzofuran-acetamides as 'antineophobic' mitochondrial DBI receptor complex ligands
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A series of novel benzofuran analogues of N,N-di-n-hexyl-2- phenylindole-3-acetamide (5, FGIN-1-27), a potent and highly specific mitochondrial DBI receptor complex ligand, were synthesized by a modified Fischer method and found in vitro and in vivo to be equally potent and selective as FGIN-1-27.
- Liao, Yi,Kozikowski, Alan P.,Guidotti, Alessandro,Costa, Erminio
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- O - substituted hydroxylamine hydrochloride and its preparation method (by machine translation)
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The present invention provides a O - substituted hydroxylamine hydrochloride and its preparation, wherein the preparation method comprises the following steps: step S1, to the acetyl hydroximic acid ethyl ester in ethanol solution of adding sodium hydroxide, in addition at the same time instillment halohydrocarbon, chloride or acyl chloride substitution reaction to take place, then added to the water in order to separate out the O - substituted [...]; step S2, the said O - substituted [...] adding hydrochloric acid solution in order to produce reflux reaction O - substituted hydroxylamine hydrochloride. According to the embodiment of the invention of the O - substituted hydroxylamine hydrochloride of the preparation method, high purity of the product can be obtained, and the method is safe, easy to process, the process is simple, and is suitable for industrial production. (by machine translation)
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Paragraph 0093; 0096; 0097
(2018/10/11)
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- NOVEL VASCULAR LEAKAGEAGE INHIBITOR
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The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present invention inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, and enhances the cortical actin ring structure, thereby inhibiting vascular leakage. Accordingly, the vascular leakage inhibitor of the present invention can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present invention is synthesized from commercially available or easily synthesizable pregnenolones, it has remarkably superior feasibility of commercial synthesis.
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Paragraph 0126
(2015/01/07)
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- Direct preparation of benzofurans from O-arylhydroxylamines
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Reaction of O-arylhydroxylamine hydrochlorides with either cyclic or acyclic ketones in the presence of methanesulfonic acid leads directly to the benzofuran derivative via a proposed one-pot condensation-rearrangement- cyclisation reaction sequence in good to excellent yields. Georg Thieme Verlag Stuttgart.
- Contiero, Fanny,Jones, Kevin M.,Matts, Edward A.,Porzelle, Achim,Tomkinson, Nicholas C.O.
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scheme or table
p. 3003 - 3006
(2010/03/03)
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- Inhibitors of transthyretin amyloid fibril formation
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Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.
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Page/Page column 8; sheet 6
(2008/06/13)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Nucleophilic Aromatic Substitution on Tricarbonyl(halogenoarene)chromium Complexes: A New Synthesis of O-Arylhydroxylamines
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A series of O-arylhydroxylamines 4 have been synthesized under mild conditions and in good yields by the reaction of tricarbonyl(halogenoarene)chromium complexes 1 with N-(tert-butyloxycarbonyl)hydroxylamine (tert-butyl N-hydroxycarbamate), followed by decomplexation and acidic hydrolysis of the tert-butyl N-(aryloxy)carbamates 3.
- Baldoli, Clara,Buttero, Paola Del,Licandro, Emanuela,Maiorana, Stefano
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p. 344 - 345
(2007/10/02)
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- Synthesis of Phenoxyamines
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Treatment of phenols with 2,4-dinitrophenoxyamine leads to the synthesis of phenoxyamines through an amine exchange reaction.Yields for this reaction are sensitive to the pKa of the phenol in a manner explainable in terms of a competing bimolecular decomposition reaction involving the 2,4-dinitrophenoxyamines.By use of an appropriately sustituted phenol, this phenomenon can be exploited to give high yields of phenoxyamines having oxygenated substitution patterns that were unattainable by previous methods.
- Castellino, Angelo J.,Rapoport, Henry
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p. 1348 - 1352
(2007/10/02)
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